GSK2973980A

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 555128

CAS#: 1414797-35-5

Description: GSK2973980A is a potent and selective DGAT1 inhibitor (hDGAT1 LE IC50 = 3 nM). GSK2973980A demonstrates excellent DMPK profiles and in vivo efficacy in a postprandial lipid excursion model in mice. Based on the overall biological and developability profiles and acceptable safety profiles in the 7-day toxicity studies in rats and dogs, GSK2973980A was selected as a candidate compound for further development in the treatment of metabolic disorders.

Chemical Structure

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GSK2973980A
CAS# 1414797-35-5
Instruction

Theoretical Analysis

MedKoo Cat#: 555128
Name: GSK2973980A
CAS#: 1414797-35-5
Chemical Formula: C25H19F5N4O4
Exact Mass: 534.13
Molecular Weight: 34.443
Elemental Analysis: C, 56.18; H, 3.58; F, 17.77; N, 10.48; O, 11.97

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

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Synonym: GSK2973980A; GSK-2973980A; GSK 2973980A;

IUPAC/Chemical Name: (S)-2-(6-(5-(3-(3,4-difluorophenyl)ureido)pyrazin-2-yl)-1-oxo-2-(2,2,2-trifluoroethyl)-1,2,3,4-tetrahydronaphthalen-2-yl)acetic acid

InChi Key: OTKTZEZTFCAULO-DEOSSOPVSA-N

InChi Code: InChI=1S/C25H19F5N4O4/c26-17-4-2-15(8-18(17)27)33-23(38)34-20-11-31-19(10-32-20)14-1-3-16-13(7-14)5-6-24(22(16)37,9-21(35)36)12-25(28,29)30/h1-4,7-8,10-11H,5-6,9,12H2,(H,35,36)(H2,32,33,34,38)/t24-/m0/s1

SMILES Code: O=C(O)C[C@@](CCC1=C2C=CC(C3=NC=C(NC(NC4=CC=C(F)C(F)=C4)=O)N=C3)=C1)(CC(F)(F)F)C2=O

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info: Acyl-CoA:diacylglycerol acyltransferase 1 (DGAT1) plays an important role in triglyceride synthesis and is a target of interest for the treatment of metabolic disorders

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 34.44 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

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Discovery of Tetralones as Potent and Selective Inhibitors of Acyl-CoA:Diacylglycerol Acyltransferase 1
Mui Cheung, Raghuram S. Tangirala, Sridhar R. Bethi, Hemant V. Joshi, Jennifer L. Ariazi, Vijaya G. Tirunagaru, and Sanjay Kumar
Publication Date (Web): January 16, 2018 (Letter)
DOI: 10.1021/acsmedchemlett.7b00450